| Bioactivity | TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities[1]. | ||||||||||||
| Invitro | TP-064 (1 μM; 72 hours) treatment reduces the proportion of NCI-H929 cells in S and G2/M phases while increasing the G1 phase fraction[1].TP-064 (0.03-3 μM; 72 hours) treatment reduces dimethyl-BAF155 level in a dose-dependent manner in both TP-064-sensitive and -insensitive cells[1].TP-064 (10 nM-10 μM; 6 days) treatment inhibits the growth of NCI-H929, RPMI8226, and MM.1R cells in a dose-dependent manner, but had no effect on acute myeloid leukemia, colon cancer, or lung cancer cell lines[1]. Cell Cycle Analysis[1] Cell Line: | ||||||||||||
| In Vivo | TP-064 (10 mg/kg; i.p.; 3 times in 5 days) induces peritonitis-associated neutrophilia in C57BL/6 mice[2]. | ||||||||||||
| Name | TP-064 | ||||||||||||
| CAS | 2080306-20-1 | ||||||||||||
| Formula | C28H34N4O2 | ||||||||||||
| Molar Mass | 458.60 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kazuhide Nakayama, et al. TP-064, a potent and selective small molecule inhibitor of PRMT4 for multiple myeloma. Oncotarget. 2018 Apr 6;9(26):18480-18493. [2]. Yiheng Zhang, et al. PRMT4 inhibitor TP-064 inhibits the pro-inflammatory macrophage lipopolysaccharide response in vitro and ex vivo and induces peritonitis-associated neutrophilia in vivo. Biochim Biophys Acta Mol Basis Dis. 2021 Jul 24;1867(11):166212. |